Palonosetron

Palonosetron

File:Palonosetron.svg
File:Palenosetron 3D.png
Clinical data
Pregnancy category	AU: B1 US: B (No risk in non-human studies)
Routes of administration	Intravenous
ATC code	A04AA05 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	Low (oral)
Protein binding	62%
Metabolism	Hepatic, 50% (mostly CYP2D6-mediated, CYP3A4 and CYP1A2 also involved)
Elimination half-life	Approximately 40 hours
Excretion	Renal, 80% (of which 49% unchanged)
Identifiers
IUPAC name (3aR)-2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3a, 4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one
CAS Number	119904-90-4
PubChem CID	148211
DrugBank	APRD00351
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C19H24N2O
Molar mass	296.407 g/mol

Palonosetron (INN, trade name Aloxi) is a 5-HT₃ antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is the most effective of the 5-HT₃ antagonists in controlling delayed CINV—nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy—and is the only drug of its class approved for this use by the U.S. Food and Drug Administration. As of 2007, it is the most recent 5-HT₃ antagonist to enter clinical use.

Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy. An oral formulation is in Phase III clinical trials.

References

Template:5-HT3 antagonists